vesicle

Hydroxy-Dynasore (Dyngo-4a) , a effective dynamin inhibitor, inhibits withDynI (brain), DynI (rec), and DynII (rec) of IC50 of 0.38 μM, 1.1 μM, and 2.3 μM, respectively.

Fructose-arginine is a non-saponin molecule from Korean Red Ginseng that attenuates AIM2 inflammatory vesicle activation.

AAK1-IN-1 (example 123) is an AAK1 (adaptor associated kinase 1) inhibitor with an IC50 of 2.2 nM. AAK1-IN-1 can be used for neurodegenerative diseases research[1]. Adaptor associated kinase 1 (AAK1) is a member of the Arkl Prkl family of serine threonine kinases. AAKl mRNA exists in two splice forms termed short and long. The long form predominates and is highly expressed in brain and heart. AAKl is enriched in synaptosomal preparations and is co-localized with endocytic structures in cultured cells. AAKl modulates clatherin coated endocytosis, a process that is important in synaptic vesicle recycling and receptor-mediated endocytosis[1]. [1]. Guanglin Luo, et al. Biaryl kinase inhibitors. WO2015153720A1.

Levetiracetam (SIB-S1) is a relatively unique anticonvulsant that is typically used in combination with other antiepileptic medications for partial onset seizures. Levetiracetam has been linked to rare instances of serum aminotransferase and alkaline phosphatase elevations during treatment and to rare cases of clinically apparent drug induced liver disease.

Tetrabenazine (Ro 1-9569) is a former antipsychotic drug used to treat various movement disorders. It inhibits neurotransmitter uptake into adrenergic storage vesicles and serves as a high-affinity label for the vesicle transport system.

S-23 ((S)-3-(4-chloro-3-fluorophenoxy)-N-(4-cyano-3-(trifluoromethyl)phenyl)-2-hydroxy-2-methylpropanamide) is an oral selective androgen receptor modulator (SARM) with a Ki of 1.7 nM. S-23 increases prostate, seminal vesicle, and levator ani muscle weights in castrated rats.

Guanosine 5'-triphosphate trisodium salt (5'-GTP trisodium salt) activates signal-transducing G proteins involved in cellular processes such as proliferation, differentiation, and activation of intracellular kinase cascades. It regulates proliferation and apoptosis through the hydrolysis by small GTPases Ras and Rho, and plays a role in vesicle docking, fusion, and formation via Rab. Additionally, GTP serves as an energy-rich precursor for the biosynthesis of DNA and RNA.

Diclofop-methyl is a common post-growth herbicide commonly used in agriculture. It enhances proton permeability of isolated oat root vesicle membranes.

DDD01035881 is a novel and highly potent anti-malarial drug that blocks parasite-to-mosquito transmission with nanomolar activity by targeting the Plasmodium vesicle membrane protein Pfs16 and blocking the formation of male gametes in the life cycle of the malaria parasite.

Desmosterol (24-Dehydrocholesterol) is a cholesterol biosynthesis intermediate that inhibits macrophage inflammatory vesicle activation and prevents vascular inflammation and atherosclerosis.

Guanosine triphosphate tritris (GTP tritris) serves as a crucial enhancer in myocyte differentiation, playing an essential role in regulating miRNA-muscle regulatory factors. It promotes the release of exosomes rich in guanine and guanine-derived molecules, and is considered an activation precursor for RNA synthesis. In mitochondrial functionality, GTP is involved in the entry of proteins into the matrix, which is vital for various regulatory pathways. It initiates peptide synthesis by facilitating the binding of formylmethionine-tRNA to the ribosome, and aids in polypeptide chain elongation. Additionally, GTP acts as a carrier for phosphates and pyrophosphates, channeling chemical energy into specific biosynthetic pathways. It activates signal transduction G proteins, regulates cellular processes such as proliferation and differentiation, and its hydrolysis by small GTPases (including Ras and Rho) is indispensable for both proliferation and apoptosis. Furthermore, the small GTPase Rab assists in vesicle docking, fusion, and formation. Beyond signal transduction, GTP is also an energy-rich precursor in the biosynthesis of DNA and RNA enzymes.

ICI-118233 is a selective inhibitor of the dense vesicle-type cyclic AMP phosphodiesterase found in liver tissue.

Brivaracetam (αR,4R) is a third-generation antiepileptic drug and anticonvulsant compound frequently used in combination with other antiepileptic compounds for the treatment of partial-onset seizures. It acts as a high-affinity ligand for synaptic vesicle protein 2A, reducing neurotransmitter release by binding to synaptic vesicle glycoprotein SV2A. Brivaracetam (αR,4R) is primarily metabolized into inactive metabolites through hydrolysis by amidase.

VICENISTATIN is a novel compound capable of inducing the vesiculation of early endosomes. It promotes the formation of vesicle-like structures by activating the Rab5-PAS pathway and enhancing membrane fluidity. Additionally, VICENISTATIN functions as an antitumor antibiotic, demonstrating antitumor activity against human colon cancer Co-3 in xenograft models.

1-Oleoyl-sn-glycero-2,3-cyclic-phosphate ammonium (18:1 Cyclic LPA) is a cyclic lysophosphatidic acid used in lipid vesicle (liposome) formation.

Dynamin I inhibitor

Tetrabenazine methanesulfonate is a medicine formerly utilized as an antipsychotic and therapy for various movement disorders. Tetrabenazine methanesulfonate blocks neurotransmitter uptake into adrenergic storage vesicles and has been used as a high-affin

Pitstop2 is an amphipathic protein-bound inhibitor of the clathrin terminal domain (IC50=12 μM) with selectivity. Pitstop2 severely interferes with receptor-mediated endocytosis, HIV entry and synaptic vesicle cycling. Pitstop2 has antitumor activity.

Tetrabenazine Racemate (Rubigen) is a selective and reversible inhibitor of vesicular monoamine transporter-2 (VMAT-2). Tetrabenazine Racemate blocks neurotransmitter uptake into adrenergic storage vesicles and has been used as a high-affinity label for the vesicle transport system.

Palmitic acid-13C (C1, C2, C3, and C4 labeled) is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid is a common 16-carbon saturated fat that represents 10-20% of human dietary fat intake and comprises approximately 25 and 65% of human total plasma lipids and saturated fatty acids, respectively.1,2Acylation of palmitic acid to proteins facilitates anchoring of membrane-bound proteins to the lipid bilayer and trafficking of intracellular proteins, promotes protein-vesicle interactions, and regulates various G protein-coupled receptor functions.1Red blood cell palmitic acid levels are increased in patients with metabolic syndrome compared to patients without metabolic syndrome and are also increased in the plasma of patients with type 2 diabetes compared to individuals without diabetes.3,4 1.Fatima, S., Hu, X., Gong, R.-H., et al.Palmitic acid is an intracellular signaling molecule involved in disease developmentCell. Mol. Life Sci.76(13)2547-2557(2019) 2.Santos, M.J., López-Jurado, M., Llopis, J., et al.Influence of dietary supplementation with fish oil on plasma fatty acid composition in coronary heart disease patientsAnn. Nutr. Metab.39(1)52-62(1995) 3.Yi, L.-Z., He, J., Liang, Y.-Z., et al.Plasma fatty acid metabolic profiling and biomarkers of type 2 diabetes mellitus based on GC/MS and PLS-LDAFEBS Lett.580(30)6837-6845(2006) 4.Kabagambe, E.K., Tsai, M.Y., Hopkins, P.N., et al.Erythrocyte fatty acid composition and the metabolic syndrome: A National Heart, Lung, and Blood Institute GOLDN studyClin. Chem.54(1)154-162(2008)

AMK is an active metabolite of the neurohormone melatonin .1,2,3,4It is formed from melatoninviathe metabolic intermediate AFMK that is then deformylated by catalase or formamidase.5,6AMK scavenges singlet oxygenin vitrowhen used at a concentration of 200 μM.1It inhibits the epinephrine- and arachidonic acid-induced production of prostaglandin E2and PGD2in ovine seminal vesicle microsomes in a concentration- and time-dependent manner, as well as LPS-induced increases in COX-2 levels in RAW 264.7 macrophages when used at a concentration of 500 μM.2,3AMK (20 mg kg) decreases MPTP-induced increases in lipid peroxidation in the cytosol and mitochondria from substantia nigra and striatum in a mouse model of MPTP-induced Parkinson's disease.4 1.Schaefer, M., and Hardeland, R.The melatonin metabolite N1-acetyl-5-methoxykynuramine is a potent singlet oxygen scavengerJ. Pineal Res.46(1)49-52(2009) 2.Kelly, R.W., Amato, F., and Seamark, R.F.N-acetyl-5-methoxy kynurenamine, a brain metabolite of melatonin, is a potent inhibitor of prostaglandin biosynthesisBiochem. Biophys. Res. Commun.121(1)372-379(1984) 3.Mayo, J.C., Sainz, R.M., Tan, D.-X., et al.Anti-inflammatory actions of melatonin and its metabolites, N1-acetyl-N2-formyl-5-methoxykynuramine (AFMK) and N1-acetyl-5-methoxykynuramine (AMK), in macrophagesJ. Neuroimmunol.165(1-2)139-149(2005) 4.Tapias, V., Escames, G., López, L.C., et al.Melatonin and its brain metabolite N1-acetyl-5-methoxykynuramine prevent mitochondrial nitric oxide synthase induction in parkinsonian miceJ. Neurosci. Res.87(13)3002-3010(2009) 5.Tan, D.-X., Manchester, L.C., Reiter, R.J., et al.Melatonin directly scavenges hydrogen peroxide: A potentially new metabolic pathway of melatonin biotransformationFree Radic. Biol. Med.29(11)1177-1185(2000) 6.Hirata, F., Hayaishi, O., Tokuyama, T., et al.In vitro and in vivo formation of two new metabolites of melatoninJ. Biol. Chem.249(4)1311-1313(1974)

17α,20β-Dihydroxy-4-pregnen-3-one (17α,20β-DHP) is an endogenous, maturation-inducing steroid that stimulates oocyte maturation in female teleost species. For instance, 1 μg ml of 17α,20β-DHP induces germinal vesicle breakdown in Persian sturgeon oocytes, a key step in maturation. Gonadotropin-releasing hormone and gonadotropins (follicle-stimulating hormone and luteinizing hormone) stimulate the production of 17α,20β-DHP in vivo or in vitro. 17α,20β-DHP also influences spermiation by stimulating milt production at 5 mg kg in various male teleosts.

Endosidin-2 is an exocyst inhibitor, a cell-permeable benzylidene benzoylhydrazine, that binds to the exocyst component of the 70 kDa (EXO70) subunit of the exocyst complex (Kd = 253 μM, EXO70A1).Endosidin-2 disrupts protein translocation between the endosomes and plasma membrane, thereby facilitating translocation of proteins to the vesicle for degradation. It also inhibits recirculation of endocytosed transferrin to the plasma membrane in HeLa cells and targets multiple isoforms of mammalian EXO70, leading to dysregulation of exocytosis.Endosidin2 can be used as a tool molecule to study cytosolization.

Phosphatidic acid is a phospholipid and an intermediate in glycerolipid biosynthesis. It is a transient intermediate in the synthesis of various phospholipid species that is synthesized de novo in cells via multiple routes, including the glycerol-3 phosphate and dihydroxyacetone phosphate pathways, enzymatic conversion of phosphatidylcholine by phospholipase D, and acetylation of lysophosphatidic acid by lysoPA-acyltransferase, among others. It has roles in shaping cellular membranes, cellular signaling, vesicle fission and fusion, as well as mitochondrial division and fusion. It stimulates respiratory burst in neutrophils independent of diacylglycerol and activates monoacylglycerol acyltransferase, phospholipase C (PLC), Ras, and phosphatidylinositol 4-phosphate (PIP4) kinase in several cell lines. Phosphatidic acids (egg) is a mixture of phosphatidic acids isolated from chicken egg with fatty acids of variable chain lengths.